Pharmacology: Drug Efficacy and Potency

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Questions and Answers

Which statement best describes the relationship between efficacy and potency based on the dynamics of drug actions?

  • Efficacy defines how effectively a drug occupies a receptor.
  • Potency refers to the maximum effect a drug can produce.
  • Efficacy indicates the drug's ability to elicit a response at a lower concentration.
  • Potency measures the amount of drug needed to produce a specific effect. (correct)

What is the consequence of adding a drug that causes a right shift in the dose-response curve for an agonist?

  • The potency of the agonist decreases. (correct)
  • The efficacy of the agonist increases.
  • The effectiveness of the agonist remains unchanged.
  • The potency of the agonist increases.

Which of the following drugs would possess the same efficacy as a full agonist according to the dynamics of drug actions?

  • A drug that causes a nonparallel shift to the right.
  • A drug with lower potency than the full agonist.
  • Drugs that are distinguished as full agonists. (correct)
  • A drug with higher efficacy than the full agonist.

In the context of drug antagonism, which type of antagonist cannot be overcome by increasing the concentration of the agonist?

<p>Competitive Irreversible Antagonist (A), Non-Competitive Antagonist (B)</p> Signup and view all the answers

How does the addition of a drug that causes a leftward shift in the dose-response curve for an agonist influence the curve?

<p>It leads to an increase in the maximum response achievable. (D)</p> Signup and view all the answers

Which drug comparison method provides a quantitative analysis of different drugs acting on the same receptors?

<p>Graded dose-response curve analysis. (A)</p> Signup and view all the answers

In pharmacological terms, what defines a partial agonist in contrast to a full agonist?

<p>It activates the receptor but has lower efficacy than a full agonist. (A)</p> Signup and view all the answers

Which drug is classified as an Angiotensin Converting Enzyme Inhibitor used to lower blood pressure?

<p>Ramipril (A)</p> Signup and view all the answers

What mechanism do Angiotensin-1 Receptor Blockers like Valsartan use in treating hypertension?

<p>Blocking receptor interaction (C)</p> Signup and view all the answers

Which of the following drugs is used as a Cholinesterase Reactivator during organophosphorus poisoning?

<p>Oximes (D)</p> Signup and view all the answers

What is a mechanism used to increase mediators in a body experiencing deficiency?

<p>Inhibition of mediator uptake (C)</p> Signup and view all the answers

Which drug is an example of a Nitric Oxide donor that assists in treating angina pectoris?

<p>Nitroglycerine (D)</p> Signup and view all the answers

What does the Median-Effective-Dose (ED50) represent?

<p>The drug dose that induces a specific therapeutic response in half the population. (D)</p> Signup and view all the answers

Which drug is characterized by a low Therapeutic Index (TI)?

<p>Warfarin (C)</p> Signup and view all the answers

What is the significance of Therapeutic Drug Monitoring?

<p>It is indicated when drugs have a narrow therapeutic window. (D)</p> Signup and view all the answers

Which drug is considered to have the highest efficacy according to the comparison of drugs A, B, C, and D?

<p>Drug B (B)</p> Signup and view all the answers

What term describes the phenomenon where the response to a drug is lost after repeated administration?

<p>Tolerance (D)</p> Signup and view all the answers

Drugs A, B, C, and D cannot be compared in potency because they act on:

<p>Different receptors (C)</p> Signup and view all the answers

What term describes the situation where one drug increases the action of another drug acting on a different receptor?

<p>Synergism (A)</p> Signup and view all the answers

Which of the following correctly defines Tachyphylaxis?

<p>Acute, rapid development of tolerance to a drug. (A)</p> Signup and view all the answers

In the context of dose-response curves, which curve provides information about drug concentration in a tissue?

<p>Graded dose-response curve (A)</p> Signup and view all the answers

What does the Therapeutic Index (TI) quantify?

<p>The relationship between toxic and therapeutic doses. (C)</p> Signup and view all the answers

What characterizes a drug with a wide therapeutic window?

<p>It is generally safe and does not require monitoring. (A)</p> Signup and view all the answers

What does potentiation refer to in pharmacology?

<p>Increased potency when combined with another drug (B)</p> Signup and view all the answers

How does the quantal dose-response curve differ from the graded dose-response curve?

<p>It shows the proportion of populations that respond therapeutically. (B)</p> Signup and view all the answers

What does Refactoriness signify in drug response?

<p>Complete loss of therapeutic efficacy. (C)</p> Signup and view all the answers

Which of the following is NOT an aspect of comparing drugs A, B, C, and D?

<p>Comparing them based on the same receptor (A)</p> Signup and view all the answers

What is the primary purpose of a quantal dose-response curve?

<p>To predict the frequency of adverse reactions in a population. (B)</p> Signup and view all the answers

What do the dose-response curves of agonists and antagonists primarily illustrate?

<p>The correlation between dose and effect in pharmacology (D)</p> Signup and view all the answers

If the new dose-response curve induced by two drugs is more effective than the first drug alone, which term describes this scenario?

<p>Synergism (A)</p> Signup and view all the answers

What is termed as ‘hyper-susceptibility’ in relation to drug response?

<p>Increased responsiveness leading to exaggerated drug effects (A)</p> Signup and view all the answers

Which condition reflects an abnormal drug response due to a genetic defect?

<p>Idiosyncrasy (D)</p> Signup and view all the answers

Which type of response is characterized by skin reactions to Penicillin?

<p>Hypersensitivity reaction (D)</p> Signup and view all the answers

What describes the withdrawal symptoms following cessation of drug use?

<p>Dependence (B)</p> Signup and view all the answers

What type of communication occurs when signals pass locally from a signaling cell to a target cell?

<p>Paracrine communication (A)</p> Signup and view all the answers

What results from repeated drug administration leading to an adaptive state?

<p>Dependence (A)</p> Signup and view all the answers

In which scenario do neurotransmitters primarily act?

<p>At the synapse between neurons (B)</p> Signup and view all the answers

What distinguishes hormones from neurotransmitters?

<p>Hormones are conveyed systemically through the blood (A)</p> Signup and view all the answers

Which of the following is NOT considered a mediator in non-endocrine signaling?

<p>Atrial natriuretic peptide (C)</p> Signup and view all the answers

What condition involves upregulation or downregulation of mediators in disease states?

<p>Mediator malfunctioning (C)</p> Signup and view all the answers

What does a low Therapeutic Index (TI) indicate regarding a drug's safety?

<p>The drug requires rigorous monitoring due to proximity of effective dose to toxic dose. (A)</p> Signup and view all the answers

Which statement best describes the phenomenon of tolerance in drug administration?

<p>Tolerance reflects a gradual decrease in responsiveness necessitating higher doses to achieve the same effect. (B)</p> Signup and view all the answers

What characterizes the concept of resistance in pharmacology?

<p>A complete ineffectiveness of a drug, particularly in antibiotics or anticancer therapies. (B)</p> Signup and view all the answers

Which of the following terms best describes the immediate loss of efficacy when doses of a drug are administered in close succession?

<p>Tachyphylaxis (D)</p> Signup and view all the answers

In which situation is Therapeutic Drug Monitoring (TDM) indicated?

<p>When the difference between therapeutic and toxic dosing is minimal. (B)</p> Signup and view all the answers

What term describes an abnormal drug response that occurs due to a genetic defect?

<p>Idiosyncrasy (D)</p> Signup and view all the answers

What physiological condition emerges from an adaptive state to repeated drug use resulting in withdrawal symptoms upon cessation?

<p>Dependence (C)</p> Signup and view all the answers

Which term best describes the immune response that leads to adverse reactions such as skin rashes from a medication?

<p>Hypersensitivity Reaction (A)</p> Signup and view all the answers

What is primarily responsible for conveying signals to distant targets through the bloodstream?

<p>Hormones (C)</p> Signup and view all the answers

Which of the following accurately describes the phenomenon of increasing responsiveness to a drug leading to adverse reactions like syncope?

<p>Hyper-susceptibility (B)</p> Signup and view all the answers

Which statement accurately reflects the comparison of drug efficacy among drugs A, B, C, and D?

<p>Efficacy ranking from highest to lowest is B, A, D, C. (C)</p> Signup and view all the answers

What is the primary distinction between 'synergism' and 'potentiation' in the context of drug interactions?

<p>Synergism leads to increased efficacy, while potentiation results in increased potency. (C)</p> Signup and view all the answers

Which aspect is NOT captured by the graded dose-response curve?

<p>The proportion of a population that experiences side effects. (C)</p> Signup and view all the answers

What effect does a drug causing a slope shift to the left in the dose-response curve represent?

<p>Potentiation of the agonist's action (D)</p> Signup and view all the answers

In pharmacology, what is meant by 'quantal dose-response curve'?

<p>A representation of the percentage of a population responding to various doses of a drug. (B)</p> Signup and view all the answers

If two drugs acting on different receptors have a combined effect that is less effective than either drug alone, which term applies?

<p>Antagonism (B)</p> Signup and view all the answers

How would one characterize the effect of a Competitive Irreversible Antagonist on an agonist's dose-response curve?

<p>It decreases the maximum response achievable by the agonist (B)</p> Signup and view all the answers

Which statement best describes Partial Agonists in relation to full agonists?

<p>They achieve a maximal response lower than that of full agonists (A)</p> Signup and view all the answers

What would indicate that a drug is acting as a Competitive Reversible Antagonist?

<p>It causes a rightward shift that is overcome by increasing agonist concentration (C)</p> Signup and view all the answers

In comparing drug potency among a group, which finding demonstrates a higher potency?

<p>Drug C reaches the same level of effect as drug A at a lower dosage (D)</p> Signup and view all the answers

Flashcards

Efficacy vs. Potency

Efficacy measures the maximum effect a drug can produce, while potency describes the amount of drug needed to produce a specific effect.

Full Agonist

A drug that produces the maximum possible effect at a receptor site.

Partial Agonist

A drug that produces a less-than-maximal effect at a receptor site, even at high concentrations.

Potentiation

An increase in the effect of a drug when combined with another drug or substance.

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Antagonism

A decrease in the effect of a drug when combined with another drug or substance.

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Competitive Antagonist

A drug that competes with an agonist for the same receptor site, diminishing the drug's effect.

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Dose-Response Curve

A graph showing the relationship between the dose of a drug and the magnitude of its effect.

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What is efficacy?

The maximum effect a drug can produce.

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What is potency?

The amount of drug needed to produce a specific effect.

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How are efficacy and potency different?

Efficacy refers to the maximum response a drug can achieve, while potency refers to the drug concentration needed to produce a specific effect.

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What is an agonist?

A drug that binds to a receptor and produces an effect.

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What is an antagonist?

A drug that blocks the effect of an agonist.

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What is competitive antagonism?

When an antagonist competes with an agonist for the same receptor.

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What is non-competitive antagonism?

When an antagonist binds to a different site on the receptor, preventing the agonist from working.

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What is synergism?

When two drugs combined have a greater effect than either drug alone.

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What is potentiation?

When one drug increases the effect of another drug.

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Quantal Response

A drug's effect is either fully present or absent for each individual, with no middle ground.

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Median Effective Dose (ED50)

The drug dose required to produce a desired therapeutic effect in 50% of the population.

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Median Toxic Dose (TD50)

The drug dose that causes a specific adverse effect in 50% of the population.

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Therapeutic Index (TI)

A measure of drug safety; calculated by dividing the TD50 by the ED50.

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Narrow Therapeutic Window

A small difference between the dose that is therapeutic and the dose that causes toxicity.

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Therapeutic Drug Monitoring (TDM)

Regularly monitoring drug levels in the blood to ensure therapeutic effect and avoid toxicity.

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Tolerance

Reduced response to a drug over time with repeated use.

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Tachyphylaxis

Rapidly developing tolerance after repeated drug doses in quick succession.

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Refractoriness

Loss of therapeutic efficacy for a drug.

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Resistance

Complete loss of effectiveness to a drug; commonly seen with antibiotics or anticancer drugs.

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Drug Actions: Suppressing Mediators

Drugs can reduce the effects of excess mediators by inhibiting their synthesis, blocking their receptors, or increasing their breakdown.

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Inhibiting Mediator Synthesis

Drugs block the production of mediators, often by interfering with enzymes involved in their synthesis.

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Blocking Mediator Receptors

Drugs bind to the receptor sites for mediators, preventing them from attaching and causing their effects.

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Increasing Mediator Degradation

Drugs increase the breakdown of mediators, removing them from circulation and reducing their effects.

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Drug Actions: Enhancing Mediators

Drugs can enhance the effects of deficient mediators by increasing the mediator's levels, mimicking their action, or blocking their breakdown.

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Drug Tolerance

When the body adapts to a drug, requiring higher doses to achieve the same effect.

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Drug Intolerance

Increased sensitivity to a drug, causing exaggerated or adverse effects.

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Idiosyncrasy

An unusual or unexpected response to a drug due to a genetic difference.

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Hypersensitivity Reaction

An immune response triggered by a drug, causing symptoms like rash, asthma, or anaphylaxis.

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Habituation

Developing a psychological dependence on a drug, characterized by craving and withdrawal symptoms.

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Physical Dependence

Developing a physiological dependence on a drug, leading to withdrawal symptoms.

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Drug Addiction

A chronic, relapsing disease characterized by compulsive drug seeking and use, despite harmful consequences.

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Mediator

A chemical messenger that transmits signals within the body.

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Neurotransmitter

A chemical messenger that transmits signals between neurons.

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Hormone

A chemical messenger that travels through the bloodstream to target cells.

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Competitive Reversible Antagonist

A drug that competes with an agonist for the same receptor site, diminishing the drug's effect. Can be overcome by increasing the concentration of the agonist.

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Efficacy

The maximum effect a drug can produce, regardless of the dose.

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Potency

The amount of drug needed to produce a specific effect.

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Non-competitive Antagonism

A drug that blocks the effects of another drug by binding to a different site on the receptor, preventing the agonist from working.

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Synergism

The combined effect of two drugs is greater than the sum of their individual effects.

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Quantal Dose-Response Curve

A type of dose-response curve where the response is either fully present or absent for each individual, with no middle ground. It's used to assess the safety and efficacy of drugs.

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What is drug tolerance?

When the body adapts to a drug, requiring higher doses to achieve the same effect. It's like the body gets used to the drug and needs more to feel the same effect.

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What is a hypersensitivity reaction?

An immune response triggered by a drug, causing symptoms like rash, asthma, or anaphylaxis. It's like your immune system attacking the drug.

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What's the difference between habituation and physical dependence?

Habituation is a psychological dependence on a drug, characterized by craving and withdrawal symptoms. Physical dependence is a physiological dependence on a drug, leading to withdrawal symptoms when stopped. Habituation is about wanting the drug, while physical dependence is about needing it to function.

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Study Notes

Dynamics of Drug Actions

  • Efficacy vs. Potency: Efficacy is the maximum effect of a drug, while potency is the amount of drug needed to produce a specific effect. Potency is important for comparing drugs' relative strengths, but efficacy is crucial in selecting the best treatment option.

  • Quantitative Comparison of Drug Response: Comparing drugs with the same receptors reveals differences in their efficacy and potency. Full agonists have similar maximal effects as the reference drug, while partial agonists have a lower maximum effect. Potency differences are also noted, which show the amount of drug needed to produce the effect.

  • Potentiation: If adding a drug increases the effect of another drug, it's called potentiation.

  • Antagonism: If adding a drug decreases the effect of another drug, it's called antagonism. Competitive antagonists reduce potency, but the effect can be reversed by increasing the concentration of the agonist if the antagonist reversibly binds to the receptors involved. Non-competitive antagonists reduce efficacy, so increasing agonist concentration will not reverse the effect.

  • Different Receptors: Comparing drugs acting on different receptors reveals that their efficacy can vary even if the potency is similar.

Graded Dose-Response Curve Use

  • Used to assess drug response by examining how the response changes in relation to drug concentration.

Quantitative Comparison of Drug Effects Acting on the Same Receptor

  • Comparing agonists (B, C, E) to a full agonist (A) reveals that B, C, and E have the same maximal effect as A, but potentially different potencies. Drugs D and F are partial agonists; they have lower maximal effects, but potentially different potencies to A.

Quantitative Comparison of Drug Effects Acting on Different Receptors

  • Comparing drugs on different receptors reveals that they may have different efficacies, despite similar potency in certain situations

Quantal Dose-Response Curve

  • Used to predict drug safety by determining median effective dose (ED50) and median toxic dose (TD50). The therapeutic index (TI) is the ratio of TD50 to ED50, and a higher TI indicates a safer drug.

Factors Affecting Drug Response

  • Tolerance: A reduced response to a drug after repeated administration; may require increasing the dosage maintain a similar effect.

  • Tachyphylaxis: A rapid development of tolerance often following repeated doses occurring in quick succession.

  • Resistance: A complete loss of drug effectiveness, often in situations with antibiotics.

  • Hyper-susceptibility (Drug Intolerance): An increased response to a drug, often exaggerated or abnormal

  • Idiosyncrasy: An abnormal or unexpected reaction to a drug, often genetically linked

  • Hypersensitivity: An immune response to a drug, often causing allergic reactions like skin rashes, or anaphylaxis.

  • Dependence: A need for a drug; when stopping use, often producing withdrawal symptoms

Drugs Affecting Mediators & Transmitters of Communication

  • Modulation: Drugs affect mediator synthesis, receptor interaction or degradation to control disease states. Examples include drugs that modify neurotransmitters, hormones or other chemical messengers.

  • Drugs Suppressing Mediators: Examples like ACE inhibitors, and Angiotensin-I receptor blockers decrease mediator activity by blocking synthesis, interaction, and degradation.

  • Drugs Increasing Mediators: Examples include drugs that mimic mediator actions, stimulating synthesis or decreasing breakdown which can help with symptoms.

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